L-796449 [Ligand Id: 2689] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL278994 (L-796449) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | In vitro binding affinity for human PPAR alpha in SPA | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Agonist activity at PPARalpha | F | 7.27 | pIC50 | 53.95 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Transcriptional activation by human PPAR alpha | B | 7.74 | pEC50 | 18 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Agonist activity for Human PPAR alpha receptor in transcriptional activation assay | F | 8.39 | pEC50 | 4.1 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204] | ||||||||
| ChEMBL | Agonist activity for murine PPAR alpha receptor in transcriptional activation assay | F | 5.12 | pEC50 | 7600 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
J Med Chem (2004) 47: 4118-27 [PMID:15293980]; J Biol Chem (1999) 274: 6718-25 [PMID:10037770] |
| ChEMBL | In vitro binding affinity for human PPAR delta in SPA | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Agonist activity at PPARdelta | F | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Agonist activity for Human PPAR delta receptor in transcriptional activation assay | F | 8.1 | pEC50 | 7.9 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Binding affinity at human GST-tagged PPARdelta ligand binding domain after 1 hr by time-resolved FRET analysis | B | 8.1 | pEC50 | 7.9 | nM | EC50 | Eur J Med Chem (2012) 53: 190-202 [PMID:22534184] |
| ChEMBL | Transcriptional activation by human PPAR delta | B | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396] | ||||||||
| ChEMBL | Agonist activity for murine PPAR delta receptor in transcriptional activation assay | F | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | - | - | - | J Biol Chem (1999) 274: 6718-25 [PMID:10037770] |
| ChEMBL | In vitro binding affinity for human PPAR gamma in SPA | B | 7.03 | pIC50 | 94 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Displacement of radio-labeled full agonist from PPARgamma receptor | F | 7.03 | pIC50 | 94 | nM | IC50 | Eur J Med Chem (2011) 46: 2513-2529 [PMID:21482446] |
| ChEMBL | Agonist activity at PPARgamma | F | 7.03 | pIC50 | 93.97 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Transcriptional activation by human PPAR gamma | B | 8.05 | pEC50 | 9 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Agonist activity for Human PPAR gamma receptor in transcriptional activation assay | F | 8.28 | pEC50 | 5.2 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Agonist activity for murine PPAR gamma receptor in transcriptional activation assay | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
